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1. 发明申请

WO2003037891A1 HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3BETA INHIBITORS (GSK3 INHIBITORS) 审中-公开
标题翻译：杂多胺作为糖原合成酶激酶3β抑制剂（GSK3抑制剂）
公开(公告)号：WO2003037891A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012077
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D403/12
CPC分类号： C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxy C 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 1-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=0)-; R 21 -S(=0)p-; R 7 -S =O R 7 -S(=O)p-NH-; R 21 -S(=O)p-NH-; R 7 -C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R° is an optionally substituted heterocycle provided that -X-R 2 and/or R 3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）化合物，其N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A为6-元杂环; R 1是氢; 芳基; 甲酰基; ç<子> 1-6 烷基羰基; 任选取代的C 1-6烷基; ç<子> 1-6 烷氧基羰基; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接基原子或基团; Z是直接键或连接基原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，每个所述基团可以任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6链烯基或C 2-6炔基; ç<子> 1-6 烷氧基; ç<子> 1-6 烷硫基; ç<子> 1-6 烷氧基羰基; ç<子> 1-6 烷基羰基氧基; 羧基; 氰基; 硝基; 氨基; 单 - 或二（C 1-6烷基）氨基; 多卤代<子> 1-6 烷基; 多卤代<子> 1-6 烷氧基; 多卤代<子> 1-6 烷硫基; [R ^{21 ; [R ^{21 -C <子> 1-6 烷基; [R ^{21 -O-; [R ^{21 -S-; [R ^{21 -C（= O） - ; [R ^{21 -S（= O）p - ; R 7 -S = O R 7 -S（= O）p -NH-; [R ^{21 -S（= O）P-NH-; [R ^{7 -C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; [R ^{7 C（= O）-NH-; [R ^{21 C（= O）-NH-; -C（= NH）R ^{7 ; -C（= NH）R ^{21 ; R＆度; 是任选取代的杂环，条件是-XR 2和/或R 3不为氢;它们的用途，包含它们的药物组合物及其制备方法。}}}}}}}}}}}}

2. 发明申请

WO2006075023A3 TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：作为糖原合成酶激酶3抑制剂的三唑基嘧啶衍生物
公开(公告)号：WO2006075023A3
公开(公告)日：2006-09-28
申请号：PCT/EP2006050206
申请日：2006-01-13
申请人： JANSSEN PHARMACEUTICA NV , LOVE CHRISTOPHER JOHN , COOYMANS LUDWIG PAUL , VANDERMAESEN NELE
发明人： LOVE CHRISTOPHER JOHN , COOYMANS LUDWIG PAUL , VANDERMAESEN NELE
IPC分类号： C07D487/04 , A61K31/519 , A61P3/10
CPC分类号： C07D487/04
摘要： This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl or C 1-6 alkylcarbonyloxy; X represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents an optionally substituted cyclic system; provided that N,3-diphenyl-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-amine is not included ; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）化合物，其N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1代表氢; 芳基; 甲酰基; ç_{1-6 烷基羰基; ç_{1-6 烷基; ç_{1-6 烷氧基羰基; 被甲酰基取代的C 1-6烷基，C 1-6烷基羰基，C 1-6烷氧基羰基或C 1-6烷基羰基， / SUB>烷基羰基氧基; X代表直接键; - （CH _{2 ）_{n3 < - >或 - （CH _{2 ）_{n4 -X < SUB> -X _{图1b - ; R 2代表任选取代的环体系; 条件是不包括N，3-二苯基-3H-1,2,3-三唑并[4,5-d]嘧啶-5-胺; 它们的用途，包含它们的药物组合物以及它们的制备方法。}}}}}}}}

3. 发明申请

WO2003015776A1 2,4,5-TRISUBSTITUTED THIAZOLYL DERIVATIVES AND THEIR ANTIINFLAMMATORY ACTIVITY 审中-公开
标题翻译： 2,4,5-三唑衍生物及其抗炎活性
公开(公告)号：WO2003015776A1
公开(公告)日：2003-02-27
申请号：PCT/EP2002/008956
申请日：2002-08-09
申请人： JANSSEN PHARMACEUTICA N.V. , LOVE, Christopher, John , VAN WAUWE, Jean, Pierre, Frans , DE BRABANDER, Marc, J. , MOSES, Roger, Clive , GONCHARENKO, Mykhalyo , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , DIELS, Gaston, Stanislas, Marcella , SIBLEY, Anthony, William , NOULA, Caterina
发明人： LOVE, Christopher, John , VAN WAUWE, Jean, Pierre, Frans , DE BRABANDER, Marc, J. , MOSES, Roger, Clive , GONCHARENKO, Mykhalyo , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , DIELS, Gaston, Stanislas, Marcella , SIBLEY, Anthony, William , NOULA, Caterina
IPC分类号： A61K31/426
CPC分类号： C07D417/04 , C07D277/28 , C07D417/14
摘要： This invention concerns the use of a compound of formula (I), a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C 1-6 alkyl; C 1-6 alkyl substituted with hydroxy, carboxyl, cyano, amino, mono -or di(C 1-6 alkyl)amino, aminocarbonyl, mono -or di(C 1-6 alkyl)aminocarbonyl, C 1-6 alkyloxycarbonyl or C 1-6 alkyloxy; polyhaloC 1-4 alkyl; C 1-4 alkyloxy; cyano; amino; aminocarbonyl; mono -or di(C 1-6 alkyl)aminocarbonyl; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; H 2 N-S(=O) 2 -; mono -or di(C 1-6 alkyl)amino-S(=O) 2 ; -C(=N-R x )NR y R z ; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-α and/or IL-12.
摘要翻译：本发明涉及式（I）化合物，其N-氧化物，其药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z为卤素; C1-6烷基; 被羟基，羧基，氰基，氨基，单 - 或二（C 1-6烷基）氨基，氨基羰基，单 - 或二（C 1-6烷基）氨基羰基，C 1-6烷氧基羰基或C 1-6烷氧基取代的C 1-6烷基; polyhaloC1-4alkyl; C1-4alkyloxy; 氰基; 氨基; 羰基; 单 - 或二（C 1-6烷基）氨基羰基; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H 2 N-S（= O）2 - ; 单 - 或二（C 1-6烷基）氨基-S（= O）2; -C（= NR ）NR - [R ; Q是任选取代的碳环或任选取代的杂环; L是取代的苯基或任选取代的单环5或6元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的疾病的药物。

4. 发明申请

WO2003015773A2 2-AMINO-4,5-TRISUBSTITUTED THIAZOLYL DERIVATIVES 审中-公开
标题翻译： 2-氨基-4,5-二取代的噻唑衍生物
公开(公告)号：WO2003015773A2
公开(公告)日：2003-02-27
申请号：PCT/EP2002/008955
申请日：2002-08-09
申请人： JANSSEN PHARMACEUTICA N.V. , LOVE, Christopher, John , VAN LOMMEN, Guy, Rosalia, Eugeen , DOYON, Julien, Georges, Pierre-Olivier , BONGARTZ, Jean-Pierre, André, Marc , VAN dER AA, Marcel, Jozef, Maria , HENDRICKX, Robert, Jozef, Maria , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , COESEMANS, Erwin , BOECKX, Gustaaf, Maria
发明人： LOVE, Christopher, John , VAN LOMMEN, Guy, Rosalia, Eugeen , DOYON, Julien, Georges, Pierre-Olivier , BONGARTZ, Jean-Pierre, André, Marc , VAN dER AA, Marcel, Jozef, Maria , HENDRICKX, Robert, Jozef, Maria , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , COESEMANS, Erwin , BOECKX, Gustaaf, Maria
IPC分类号： A61K31/425
CPC分类号： C07D417/04 , C07D277/42 , C07D471/04
摘要： This invention concerns the use of a compound of formula (I'), a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C 1-6 alkyl; C 1-6 alkylcarbonyl; C 1-6 alkyloxycarbonyl; aminocarbonyl; C 1-6 alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C 1-4 alkyl substituted piperidinyl, mono -or di(C 1-6 alkyl)amino, aminocarbonyl, mono -or di(C 1-6 alkyl)aminocarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC 1-4 alkyl; cyano; amino; mono -or di(C 1-6 alkyl)aminocarbonyl; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; aminoS(=O) 2 -; mono -or di(C 1-6 alkyl)aminoS(=O) 2 ; -C(=N-R x )NR y R z ; Q is optionally substituted C 3-6 cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12.
摘要翻译：本发明涉及式（I'）化合物，其N-氧化物，其药学上可接受的加成盐，季胺及其立体化学异构形式的用途，其中Z为卤素; C1-6烷基; C1-6烷基; C1-6alkyloxycarbonyl; 羰基; 被羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单 - 或二（C 1-6烷基）氨基，氨基羰基，单 - 或二（C 1-6烷基）氨基羰基 C 1-6烷氧基羰基，C 1-6烷氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; polyhaloC1-4alkyl; 氰基; 氨基; 单 - 或二（C 1-6烷基）氨基羰基; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS（= O）2 - ; 单 - 或二（C 1-6烷基）氨基S（= O）2; -C（= NR ）NR - [R ; Q是任选取代的C 3-6环烷基，苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基，或Q是式（b-1），（b-2） b-3），L是任选取代的苯基或任选取代的单环5或6元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的炎症和/或自身免疫疾病的药物。

5. 发明申请

WO2007003525A3 CYCLIC ANILINO-PYRIDINOTRIAZINES AS GSK-3 INHIBITORS 审中-公开
标题翻译：作为GSK-3抑制剂的CYCLIC ANILINO-PYRIDINOTRIAZINES
公开(公告)号：WO2007003525A3
公开(公告)日：2008-04-10
申请号：PCT/EP2006063555
申请日：2006-06-26
申请人： JANSSEN PHARMACEUTICA NV , ROMBOUTS FREDERIK JAN RITA , LOVE CHRISTOPHER JOHN , EMELEN KRISTOF VAN , VAN BRANDT SVEN FRANCISCUS ANN , WU TONGFEI
发明人： ROMBOUTS FREDERIK JAN RITA , LOVE CHRISTOPHER JOHN , VAN EMELEN KRISTOF , VAN BRANDT SVEN FRANCISCUS ANN , WU TONGFEI
IPC分类号： C07D251/16 , A61K31/53 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08 , C07D487/18
CPC分类号： C07D487/18 , C07D251/16 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08
摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; -X 1 - represents C 1-4 alkyl, in particular methyl; -X 2 - represents -C 1-4 alkyl- or -C 1-4 alkyl-NR 7 -, in particular propyl, -ethyl-NR 7 - or -propyl-NR 7 -; -Y- represents-NR 2 -C 1-6 alkyl-CO-NR 4 -, -Het 1 -C 1-6 alkyl-CO-NR 5 - or -Het 2 -CO-NR 6 - and wherein the -C 1-6 alkyl- linker of -NR 2 -C 1-6 alkyl-CO-NR 4 - or -Het 1 -C 1-6 alkyl-CO-NR 5 - is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R 1 represents hydrogen, chloro, fluoro or bromo; R 2 represents -C 1-4 alkyl-, in particular ethyl or methyl; R 7 represents hydrogen; R 8 represents hydrogen; R 4 , R 5 and R 6 represent hydrogen; Het 1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het 2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中m表示1，n表示1，Z表示N或C，特别是N; -X 1表示C 1-4烷基，特别是甲基; -X 2 - 表示-C 1-4烷基 - 或-C 1-4 - 烷基-NR 7 - - ，特别是丙基， - 乙基 - NR 7 - 或 - 丙基-NR 7 - 。 -Y-表示-NR 2 -C 1-6烷基-CO-NR 4 - ，-Het 1 SUP / > -C 1-6烷基-CO-NR 5 - 或-Het 2 -CO-NR 6 - - 并且其中-NR 2 -C 1-6烷基-CO-NR的-C 1-6烷基 - 连接基团， 4 - 或-Het 1 -C 1-6烷基-CO-NR 5 - 任选被一个或多个可能的两个或更多个选自羟基，卤素和苯基的取代基; R 1表示氢，氯，氟或溴; R 2表示-C 1-4烷基 - ，特别是乙基或甲基; R 7表示氢; R 8表示氢; R 4，R 5和R 6表示氢; Het 1选自哌嗪基或哌啶基，特别是哌嗪基; Het 2选自吡咯烷基或哌啶基，特别是吡咯烷基，其中所述吡咯烷基任选被羟基取代。

6. 发明申请

WO03037891A8 HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3BETA INHIBITORS (GSK3 INHIBITORS) 审中-公开
标题翻译：作为GLYCOGEN SYNTHASE KINASE 3BETA抑制剂（GSK3抑制剂）的HETEROARYL AMINES
公开(公告)号：WO03037891A8
公开(公告)日：2003-09-04
申请号：PCT/EP0212077
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA NV , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , LOVE CHRISTOPHER JOHN , JANSSEN PAUL ADRIAAN JAN , LEWI PAULUS JOANNES , HEERES JAN , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , VAN AKEN KOEN JEANNE ALFONS , DIELS GASTON STANISLAS MARCELL
发明人： FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , LOVE CHRISTOPHER JOHN , JANSSEN PAUL ADRIAAN JAN , LEWI PAULUS JOANNES , HEERES JAN , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , VAN AKEN KOEN JEANNE ALFONS , DIELS GASTON STANISLAS MARCELL
IPC分类号： A61K31/435 , A61K31/4406 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P17/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , C07D213/53 , C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxy C1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C1-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21-O-; R21-S-; R21-C(=0)-; R21-S(=0)p-; R7-S =O R7-S(=O)p-NH-; R21-S(=O)p-NH-; R7-C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R21; R° is an optionally substituted heterocycle provided that -X-R2 and/or R3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A为6-元杂环; R1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C 1-6烷基; R21-O-; R21-S-; R21-C（= O） - ; R21-S（= O）p - ; R7-S = O R7-S（= O）p-NH-; R21-S（= O）P-NH-; R7-C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R7-C（= O）-NH-; R21-C（= O）-NH-; -C（= NH）R 7; -C（= NH）R 21; R°是任选取代的杂环，条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

7. 发明申请

WO1997043279A1 2,4-DIAMINOPYRIMIDINE DERIVATES AS DOPAMINE D4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2,4-二氨基吡啶衍生物作为DOPAMINE D4受体拮抗剂
公开(公告)号：WO1997043279A1
公开(公告)日：1997-11-20
申请号：PCT/EP1997002506
申请日：1997-05-02
申请人： JANSSEN PHARMACEUTICA N.V. , BOSMANS, Jean-Paul, René, Marie, André , LOVE, Christopher, John , VAN LOMMEN, Guy, Rosalia, Eugène
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl or C3-6alkenediyl; R is hydrogen or C1-4alkyl; R and R each independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; or R and R may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R is hydrogen or halo; Q is aryl, aryloxy, di(aryl)methyl or heteroaryl; aryl is naphthyl or phenyl, said naphthyl and phenyl may optionally be substituted; and heteroaryl is quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4-benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl; said heteroaryls may optionally be substituted; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的酸加成盐和立体化学异构形式，其中Alk是C 1-6烷二基或C 3-6亚烯基; R 1是氢或C 1-4烷基; R 2和R 3各自独立地为氢，C 1-6烷基或C 3-7环烷基; 或R 2和R 3也可以与它们所连接的氮原子一起，从而形成吡咯烷，哌啶或全氢氮杂环; R 4是氢或卤素; Q是芳基，芳氧基，二（芳基）甲基或杂芳基; 芳基是萘基或苯基，所述萘基和苯基可任选被取代; 异喹啉基，吡啶基，噻吩基，吲哚基，2,3-二氢-1,4-苯并二氧杂环己基，2,3-二氢 - 苯并呋喃基或苯并二氧杂环戊烷基; 所述杂芳基可任选被取代; 它还涉及它们的制备方法，包含它们的组合物以及它们作为药物的用途; 含有放射性同位素的式（I）化合物; 标记多巴胺D4受体位点的过程; 并且公开了用于成像器官的方法。

8. 发明申请

WO2009132000A1 QUINOLINE OR ISOQUINOLINE SUBSTITUTED P2X7 ANTAGONISTS 审中-公开
标题翻译：喹啉或异喹啉取代P2X7拮抗剂
公开(公告)号：WO2009132000A1
公开(公告)日：2009-10-29
申请号：PCT/US2009/041249
申请日：2009-04-21
申请人： JANSSEN PHARMACEUTICA NV , LOVE, Christopher, John , LEENAERTS, Joseph, Elisabeth , COOYMANS, Ludwig, Paul , LEBSACK, Alec, Donald , BRANSTETTER, Bryan, James , RECH, Jason, Christopher , GLEASON, Elizabeth, Ann , VENABLE, Jennifer, Diane , WIENER, Danielle , SMITH, Deborah, Margaret , BREITENBUCHER, James, Guy
发明人： LOVE, Christopher, John , LEENAERTS, Joseph, Elisabeth , COOYMANS, Ludwig, Paul , LEBSACK, Alec, Donald , BRANSTETTER, Bryan, James , RECH, Jason, Christopher , GLEASON, Elizabeth, Ann , VENABLE, Jennifer, Diane , WIENER, Danielle , SMITH, Deborah, Margaret , BREITENBUCHER, James, Guy
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , A61K31/4427
CPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/08
摘要： The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I)
摘要翻译：本发明涉及具有P2X7拮抗性质的新型式（I）化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其用于治疗或预防与动物中P2X7受体活性有关的疾病的用途，特别是人类。（一世）

9. 发明申请

WO2005012307A1 TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂
公开(公告)号：WO2005012307A1
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051455
申请日：2004-07-12
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy Jean Edgard , LOVE, Christopher John , COOYMANS, Ludwig Paul , VANDERMAESEN, Nele , BUIJNSTERS, Peter Jacobus Johannes Antonius , WILLEMS, Marc , EMBRECHTS, Werner Constant Johan
发明人： FREYNE, Eddy Jean Edgard , LOVE, Christopher John , COOYMANS, Ludwig Paul , VANDERMAESEN, Nele , BUIJNSTERS, Peter Jacobus Johannes Antonius , WILLEMS, Marc , EMBRECHTS, Werner Constant Johan
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention concerns a compound of formula (I), a N -oxide, a pharmaceutically acceptable addition salt, a quaternary arnine and a stereochernic ally isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyI; C l . 6 alkylcarbonyl, C 1-6 alkyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylearbonyl, C 1-6 alkyloxycarbonyl, C 1 - 6 alkylcarbonyloxy; or C 1 - 6 alkyloxyC 1-6 alkylcarbonyl optionally substituted with C 1-6 alkyloxycarbonyl; X represents a direct bond; -(CH 2 ) n3 or -(CH 2 ) m4 -X 1a -X 1b -; R 2 represents C 3-7 cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatom. selected from 0, S or N; benzoxazolyl or a radical of formula (a-1), wherein said R 2 substituent may optionally be substituted; R 3 represents halo; hydroxy; optionally substituted C 1-.6 alkyl; C 2-6 a]kenyl or C 2-6 alkynyl, each optionally substituted; optionally substituted polyhaloC 1-6 alkyl; optionally substituted C 1-6 alkyloxy; optionally substituted polyhaloC 1-6 alkyloxy; C 1-6 alkylthio; polyhaloC 1-6 a]kylthio; C 1-6 a]kyloxycarbonyl; C 1-6 alkylcarbonyloxy; C 1-6 alkylearbonyl; polyhaloC 1-6 alkylcarbonyl; cyano; carboxyl; aryloxy; arylthio; arylcarbonyl; NR 6b R 7b ; C(=O)-NR 6b R 7b ; -NR 5 -C(=O)R 5 ;'-S(=O) nl -R 8a ; -NR 5 S(=O) nl -R 8a ;-NR 5 -S(=O) nl -R 8a ; -S-CN; -NR 5 -CN;R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; C 2-4 alkenyl or C 2-4 alkynyl, each optionally substituted; polyha]oC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhalo-C 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhatoC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 10 R 11 ; C(=O)NR 10 -R 11 ;NR 5 -C(=O)-NR 10 R 11 ;-NR 5 -C(=O)-R 5 ; -S(=O) nl ,-R 12 -NR 5 -S(=O) nI -R 12 ; -S-CN; -NR 5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季铵和其立体异构体异构体形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1表示氢; 芳基; 甲酰基; C 1-6烷基羰基，C 1-6烷基; C1-6alkyloxycarbonyl; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰氧基取代的C 1-6烷基; 或任选被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; X表示直接键; - （CH2）n3or - （CH2）m4-X1a-X1b-; R 2表示C 3-7环烷基; 苯基; 含有至少一个杂原子的4,5,6-或7-元单环杂环。选自0，S或N; 苯并恶唑基或式（a-1）的基团，其中所述R 2取代基可任选被取代; R 3表示卤素; 羟基; 任选取代的C 1-6烷基; C 2-6烯基或C 2-6炔基，各自任选取代; 任选取代的多卤代C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的多卤代C 1-6烷氧基; C 1-6烷; polyhaloC1-6a]烷硫基; C1-6a] kyloxycarbonyl; C1-6alkylcarbonyloxy; C1-6alkylearbonyl; polyhaloC1-6alkylcarbonyl; 氰基; 羧基; 芳; 芳; 基羰基; NR 6b; R 7b; C（= O）-NR 6b R 7b; -NR <5> -C（= O）R <5>;' - S（= O）NL-R <8A>; -NR 5 S（= O）n -R 8 8a; -NR 5 -S（= O）n -R 8 8a; -S-CN; -NR 5 -CN; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; C2-4烯基或C2-4炔基，各自任选取代; polyha] OC 1-3烷基; 任选取代的C 1-4烷氧基; 多卤代C1-3alkyloxy; C1-4alkylthio; 多卤代C 1-3烷硫基C 1-4烷氧基羰基; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhatoC1-4alkylcarbonyl; 硝基; 氰基; 羧基; NR 10 R 11; C（= O）NR 10 -R 11; NR 5 -C（= O）-NR 10 R 11; -NR 5 -C（= O）-R 5 >; -S（= O）n1，-R 12 -NR 5 -S（= O）n I -R 12; -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。

10. 发明申请

WO2005012304A2 TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂
公开(公告)号：WO2005012304A2
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051457
申请日：2004-07-12
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , LOVE, Christopher, John , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan
发明人： FREYNE, Eddy, Jean, Edgard , LOVE, Christopher, John , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan
IPC分类号： C07D487/00
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochernically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 a]kyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonytoxy; or optionally substituted C 1-6 alkyloxyCl-6alkylcarbonyl; X 1 represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents optionally substituted C 3-7 CYCloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X 2 represents a direct bond; -NR 1 -NR 1 -(CH 2 ) N3 -; -0-; -0-(CH 2 ) n3 -; -C(=O)-; -C(=O)- (CH 2 ) n3 -; -C(=O)-NR 5 -(CH 2 ) n3 -; -C(=S)-; -S-; -S(=O) n1 -; -(CH 2 ) n3 -; -(CH 2 ) n4 -X 1a -X 1b -; -X 1a .-X 1b -(CH 2 ) n4 -; -S(=O) n1 -NR 5 -(CH 2 ) n3 -NR 5 _ or -S(=O) n1 ,-NR 5 -(CH 2 ) n3 -; R 3 represents an optionally substituted 5-or 6-membered monocyclic heterocycle containing at least one heteroatom selected from 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, S or N; R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; optionally substituted C 2-4 alkenyl or C 2-4 alkynyl; polyhaloC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhaloC 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio; C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhaloC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 9 R 10 ; C(=O)NR 9 R 10 ;-NR 5_ C(=O)-NR 9 R 10 ; -NR 5 -C(=O)-R 5 ; -S(=O) n1 ,-R 11 -NR 5 -S(=O) n1 ,-R 11 -S-CN; -NR 5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体异构体形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1表示氢; 芳基; 甲酰基; C 1-6烷基羰基; C 1-6 a] kyl; C 1-6烷氧基羰基; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基氧基取代的C 1-6烷基; 或任选取代的C 1-6烷氧基C 1-6烷基羰基; X1表示直接键; - （CH 2）n3-或 - （CH 2）n4-X1a-X1b-; R 2表示任选取代的C 3-7C环烷基; 苯基; 含有至少一个选自0，S或N的杂化剂的4,5,6-或7-元单环杂环; 苯并恶唑基或式（a-1）基团; X2表示直接键; -NR 1 -NR 1 - （CH 2）N 3 - ; -0-; -O-（CH 2）N 3 - ; -C（= O） - ; -C（= O） - （CH 2）n3-; -C（= O）-NR <5> - （CH2）N3-; -C（= S） - ; -S-; -S（= O）N 1 - ; - （CH2）N3-; - （CH 2）N 4 - X1A-X1b-; -X1a.-X1b-（CH2）N4-; -S（= O）n1-NR5 - （CH2）n3-NR5或-S（= O）n1，-NR5 - （CH2）n3-; R 3表示含有至少一个选自O，S或N的杂原子或含有至少一个选自O，S或S的杂原子的9元或10元双环杂环的任选取代的5元或6元单环杂环， N; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; 任选取代的C 2-4烯基或C 2-4炔基; polyhaloC1-3alkyl; 任选取代的C 1-4烷氧基; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; 硝基; 氰基; 羧基; NR <9> - [R <10>; C（= O）NR <9> - [R <10>; - NR <5_> C（= O）-NR <9> - [R <10>; -NR <5> C（= O）-R <5>; -S（= O）n1，-R 11 -NR 5 -S（= O）n1，-R 11 -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。

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